货号:A160473
同义名:
c-Cot Kinase Inhibitor; Tumor Progression Locus 2 Kinase Inhibitor
Tpl2 Kinase Inhibitor 1是一种选择性 Tpl2(COT 激酶,MAP3K8)抑制剂,IC50 为 50 nM,可用于研究炎症反应和某些癌症的进展机制。


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|---|---|---|---|---|---|---|---|
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| 产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
98% | |||||||||||||||||
| Adezmapimod | 99%+ | ||||||||||||||||||
| Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
| Skepinone-L |
++++
p38α, IC50: 5 nM |
98% | |||||||||||||||||
| Doramapimod |
++++
p38α, IC50: 38 nM p38α, Kd: 0.1 nM |
99%+ | |||||||||||||||||
| VX-702 | 99%+ | ||||||||||||||||||
| Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
98% | |||||||||||||||||
| SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
99%+ | ||||||||||||||||
| Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
99%+ | ||||||||||||||||
| Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
99%+ | ||||||||||||||||
| PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
99% | ||||||||||||||||
| TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
99%+ | ||||||||||||||||
| SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
99%+ | ||||||||||||||||
| Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
98%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Tpl2 Kinase Inhibitor 1, a 3-pyridylmethylamino analog, selectively inhibits Tpl2 (IC50=50 nM), encompassing COT kinase and MAP3K8. It significantly contributes to controlling inflammation and the advancement of certain cancers[1][2]. |
| 体外研究 | Tpl2 (Cot/MAP3K8), a serine/threonine kinase within the MAP3K family, functions upstream of MEK in the ERK pathway[1]. Tpl2 Kinase Inhibitor 1 also targets MK2 and p38, exhibiting IC50 values of 110 μM and 180 μM, respectively, in A431 cells[1]. Tpl2 Kinase Inhibitor 1 suppresses TNF-alpha production triggered by lipopolysaccharide in primary human monocytes and whole blood, with IC50 values of 0.7 μM and 8.5 μM, respectively[1]. Cancer Osaka thyroid (COT) kinase (Tpl2) significantly regulates pro-inflammatory cytokine production in macrophages[2]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.35mL 2.47mL 1.24mL |
24.70mL 4.94mL 2.47mL |
|
| CAS号 | 871307-18-5 |
| 分子式 | C21H14ClFN6 |
| 分子量 | 404.83 |
| SMILES Code | N#CC1=C(NC2=CC=C(F)C(Cl)=C2)C3=CC(NCC4=CC=CN=C4)=NC=C3N=C1 |
| MDL No. | MFCD10566771 |
| 别名 | c-Cot Kinase Inhibitor; Tumor Progression Locus 2 Kinase Inhibitor; TC-S 7006; MAP3K8 Kinase Inhibitor; Tpl2 Kinase Inhibitor |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 105 mg/mL(259.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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